HUT74613A - 16-substituted-4-aza-androstane derivatives as 5-alpha-reductase isozyme 1 inhibitors and pharmaceutical compositions containing the same - Google Patents

16-substituted-4-aza-androstane derivatives as 5-alpha-reductase isozyme 1 inhibitors and pharmaceutical compositions containing the same Download PDF

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Publication number
HUT74613A
HUT74613A HU9601037A HU9601037A HUT74613A HU T74613 A HUT74613 A HU T74613A HU 9601037 A HU9601037 A HU 9601037A HU 9601037 A HU9601037 A HU 9601037A HU T74613 A HUT74613 A HU T74613A
Authority
HU
Hungary
Prior art keywords
aza
oxo
androstane
dimethyl
alpha
Prior art date
Application number
HU9601037A
Other languages
English (en)
Hungarian (hu)
Other versions
HU9601037D0 (en
Inventor
Philippe L Durette
William K Hagmann
Thomas J Lanza
Gary H Rasmusson
Soumya P Sahoo
Richard L Tolman
Langen Derek Von
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of HU9601037D0 publication Critical patent/HU9601037D0/hu
Publication of HUT74613A publication Critical patent/HUT74613A/hu

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
HU9601037A 1993-10-21 1994-10-21 16-substituted-4-aza-androstane derivatives as 5-alpha-reductase isozyme 1 inhibitors and pharmaceutical compositions containing the same HUT74613A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14115393A 1993-10-21 1993-10-21

Publications (2)

Publication Number Publication Date
HU9601037D0 HU9601037D0 (en) 1996-06-28
HUT74613A true HUT74613A (en) 1997-01-28

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9601037A HUT74613A (en) 1993-10-21 1994-10-21 16-substituted-4-aza-androstane derivatives as 5-alpha-reductase isozyme 1 inhibitors and pharmaceutical compositions containing the same

Country Status (29)

Country Link
US (4) US5739137A (fr)
EP (1) EP0724592B1 (fr)
JP (1) JP2862376B2 (fr)
KR (1) KR100363994B1 (fr)
CN (1) CN1058499C (fr)
AT (1) ATE175420T1 (fr)
BG (1) BG61978B1 (fr)
BR (2) BR9407866A (fr)
CA (1) CA2173863C (fr)
CY (1) CY2136B1 (fr)
CZ (1) CZ292614B6 (fr)
DE (1) DE69415824T2 (fr)
DK (1) DK0724592T3 (fr)
ES (1) ES2125495T3 (fr)
FI (1) FI961697A0 (fr)
HK (1) HK1009047A1 (fr)
HU (1) HUT74613A (fr)
IL (1) IL111357A (fr)
LV (2) LV11622B (fr)
NO (1) NO308037B1 (fr)
NZ (1) NZ275293A (fr)
PL (1) PL179611B1 (fr)
RO (1) RO116197B1 (fr)
RU (1) RU2142956C1 (fr)
SK (1) SK281645B6 (fr)
TW (1) TW413682B (fr)
UA (1) UA44257C2 (fr)
WO (1) WO1995011254A1 (fr)
ZA (1) ZA948285B (fr)

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* Cited by examiner, † Cited by third party
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US5547957A (en) 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
KR100363994B1 (ko) * 1993-10-21 2003-04-10 머크 앤드 캄파니 인코포레이티드 16-치환된-4-아자-안드로스탄5-알파-리덕타제아이소자임1억제제
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
CA2199979A1 (fr) * 1994-10-21 1996-05-02 Joanne Waldstreicher Procede combine de traitement de l'acne
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
AU704933B2 (en) * 1995-10-19 1999-05-06 Merck & Co., Inc. 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors
US5872126A (en) * 1996-09-06 1999-02-16 Merck & Co., Inc. Methods and compositions for treating preterm labor
US5945412A (en) * 1996-12-09 1999-08-31 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
US5935968A (en) 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
WO1998041509A1 (fr) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methodes et compositions de traitement de la polykystose ovarienne
JP2001521000A (ja) * 1997-10-28 2001-11-06 メルク エンド カムパニー インコーポレーテッド 誘発性急性閉尿の予防
US6187925B1 (en) * 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
AR016257A1 (es) * 1998-05-14 2001-06-20 Merck & Co Inc Proceso para la sintesis estereoselectiva de ariloxi-4-aza-5alfa-androstan-3-onas, 16 alfa y 16 beta-sustituidas e insustituidas, e intermediariosobtenidos en dicho proceso.
WO1999058550A1 (fr) * 1998-05-14 1999-11-18 Merck & Co., Inc. 7β-METHYL-16β-((4-METHYLSULFONYL)-PHENOXY)-4-AZA-5α-ANDROST-1-EN-3-ONE UTILISEE COMME INHIBITEUR D'ISO-ENZYME 5α-REDUCTASE 1
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
AU754604B2 (en) * 1998-07-29 2002-11-21 Merck & Co., Inc. Tricyclic compounds
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
US20020198215A1 (en) * 2000-10-23 2002-12-26 Lino Tavares Terazosin transdermal device and methods
EP1734963A4 (fr) * 2004-04-02 2008-06-18 Merck & Co Inc Methode destinee a traiter des hommes presentant des troubles metaboliques et anthropometriques
EP1865955A4 (fr) * 2005-03-25 2009-04-15 Merck & Co Inc Traitement d'humains de sexe masculin par supplementation en testosterone associee a un inhibiteur de 5alpha-reductase
US20060241696A1 (en) * 2005-04-26 2006-10-26 Stjepan Krco Method of limiting hair loss and promoting hair growth
FR2910002B1 (fr) * 2006-12-13 2009-01-30 Sanofi Aventis Sa Nouveau procede pour l'obtention diastereoselective d'une amine primaire chirale sur un steroide
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
TWI593411B (zh) 2013-04-30 2017-08-01 徐懷山 組合物於製備抑制雄性素受體有關之功能及治療雄性素 受體相關之疾病的藥物之用途

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AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
US4220775A (en) * 1979-03-15 1980-09-02 Merck & Co., Inc. Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors
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US5120742A (en) * 1984-02-27 1992-06-09 Merck & Co., Inc. 17 β-acyl-4-aza-5 α-androst-1-ene-3-ones as 5 α-reductase inhibitors
US5151429A (en) * 1984-02-27 1992-09-29 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α reductase inhibitors
US5571817A (en) * 1984-02-27 1996-11-05 Merck & Co., Inc. Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
US4859681A (en) * 1984-02-27 1989-08-22 Merck & Co., Inc. 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors
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DE3888378T2 (de) * 1987-04-03 1994-09-29 Merck & Co Inc Behandlung von Prostatacarcinoma mit 17-beta-n-monosubstituierten-Carbamoyl-4-aza-5-alpha-Androst-1-en-3-onen.
EP0285382B1 (fr) * 1987-04-03 1994-04-13 Merck & Co. Inc. Traitement d'alopécia androgénique avec 17-bêta-n-monosubstitué-carbamoyl-4-aza-5-alpha-androst-1-en-3-ones
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CA2084798A1 (fr) * 1991-12-17 1993-06-18 Glenn J. Gormley Methode de prevention du carcinome prostatique a l'aide de 17beta -acyl -4-a-za-5.-androst-1-ene-3-ones
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KR950701527A (ko) * 1992-05-21 1995-04-28 라브리 페르낭 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY)
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US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
KR100363994B1 (ko) * 1993-10-21 2003-04-10 머크 앤드 캄파니 인코포레이티드 16-치환된-4-아자-안드로스탄5-알파-리덕타제아이소자임1억제제
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
US5512555A (en) * 1994-07-21 1996-04-30 Merck & Co., Inc. Method of treating sweat-related conditions using finasteride, epristeride and a cholestan-3-one
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents

Also Published As

Publication number Publication date
NO961575D0 (no) 1996-04-19
TW413682B (en) 2000-12-01
DE69415824T2 (de) 1999-08-05
US5910497A (en) 1999-06-08
KR960705839A (ko) 1996-11-08
LV12316A (lv) 1999-07-20
DK0724592T3 (da) 1999-08-30
US5739137A (en) 1998-04-14
EP0724592B1 (fr) 1999-01-07
US5719158A (en) 1998-02-17
WO1995011254A1 (fr) 1995-04-27
AU680063B2 (en) 1997-07-17
ATE175420T1 (de) 1999-01-15
RO116197B1 (ro) 2000-11-30
BR9407866A (pt) 1996-10-29
EP0724592A1 (fr) 1996-08-07
HU9601037D0 (en) 1996-06-28
US6204273B1 (en) 2001-03-20
CN1136318A (zh) 1996-11-20
IL111357A0 (en) 1994-12-29
CZ122896A3 (en) 1997-01-15
JPH09511213A (ja) 1997-11-11
CY2136B1 (en) 2002-06-21
BG100516A (en) 1996-11-29
NO308037B1 (no) 2000-07-10
CA2173863C (fr) 2003-05-13
CN1058499C (zh) 2000-11-15
BR1100217A (pt) 1999-11-09
FI961697A (fi) 1996-04-18
LV11622A (lv) 1996-12-20
SK49696A3 (en) 1996-10-02
FI961697A0 (fi) 1996-04-18
IL111357A (en) 2001-01-28
PL179611B1 (pl) 2000-10-31
PL314039A1 (en) 1996-08-05
KR100363994B1 (ko) 2003-04-10
LV11622B (en) 1997-06-20
NZ275293A (en) 1998-02-26
NO961575L (no) 1996-04-19
RU2142956C1 (ru) 1999-12-20
AU8086194A (en) 1995-05-08
HK1009047A1 (en) 1999-05-21
ES2125495T3 (es) 1999-03-01
LV12316B (en) 1999-11-20
CZ292614B6 (cs) 2003-11-12
UA44257C2 (uk) 2002-02-15
JP2862376B2 (ja) 1999-03-03
SK281645B6 (sk) 2001-06-11
ZA948285B (en) 1995-06-19
BG61978B1 (bg) 1998-11-30
CA2173863A1 (fr) 1995-04-27
DE69415824D1 (de) 1999-02-18

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